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Nature Chemical Biology
Article
License: implied-oa
Data sources: UnpayWall
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PubMed Central
Other literature type . 2015
Data sources: PubMed Central
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Nature Chemical Biology
Article . 2015 . Peer-reviewed
License: Springer TDM
Data sources: Crossref
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Structural mechanism underlying capsaicin binding and activation of the TRPV1 ion channel

Authors: Yang, Fan; Xiao, Xian; Cheng, Wei; Yang, Wei; Yu, Peilin; Song, Zhenzhen; Yarov-Yarovoy, Vladimir; +1 Authors

Structural mechanism underlying capsaicin binding and activation of the TRPV1 ion channel

Abstract

Capsaicin bestows spiciness by activating TRPV1 channel with exquisite potency and selectivity. Although a capsaicin-bound channel structure was previously resolved by cryo-EM at 4.2- to 4.5-Å resolution, capsaicin was registered as a small electron density, reflecting neither its chemical structure nor specific ligand-channel interactions--important details required for mechanistic understanding. We obtained the missing atomic-level details by iterative computation and confirmed them by systematic site-specific functional tests. We observed that the bound capsaicin takes a 'tail-up, head-down' configuration. The vanillyl and amide groups form specific interactions to anchor its bound position, while the aliphatic tail may sample a range of conformations, making it invisible in cryo-EM images. Capsaicin stabilizes TRPV1's open state by 'pull-and-contact' interactions between the vanillyl group and the S4-S5 linker. Our study provides a structural mechanism for the agonistic function of capsaicin and its analogs, and demonstrates an effective approach to obtain atomic-level information from cryo-EM structures.

Country
United States
Related Organizations
Keywords

Biochemistry & Molecular Biology, Patch-Clamp Techniques, Recombinant Fusion Proteins, Molecular Sequence Data, Sequence Homology, TRPV Cation Channels, Gene Expression, Article, Medicinal and Biomolecular Chemistry, Mice, Species Specificity, Bacterial Proteins, Animals, Humans, Point Mutation, Amino Acid Sequence, Dental/Oral and Craniofacial Disease, Pain Research, Cryoelectron Microscopy, Rats, Molecular Docking Simulation, Amino Acid, Kinetics, Luminescent Proteins, HEK293 Cells, Biochemistry and Cell Biology, Rabbits, Capsaicin, Sequence Alignment, Chickens, Ion Channel Gating, Protein Binding

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    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
273
Top 1%
Top 10%
Top 1%
Green
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